Evidence mapPaperPMID 40362377Full record

ArticleInternational journal of molecular sciences2025

Acridine-Based Chalcone 1C and ABC Transporters.

Ondrej Franko, Martina Čižmáriková, Martin Kello, Radka Michalková, Olga Wesołowska, Kamila Środa-Pomianek, Sérgio M Marques, David Bednář, Viktória Háziková, Tomáš Ján Liška and 1 more

Abstract read
In one paragraph

Article in International journal of molecular sciences, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors.

Ondrej FrankoDepartment of Pharmacology, Faculty of Medicine, Pavol Jozef Šafárik University, 040 11 Košice, Slovakia.
Martina ČižmárikováDepartment of Pharmacology, Faculty of Medicine, Pavol Jozef Šafárik University, 040 11 Košice, Slovakia.ORCID 0000-0002-1158-6161
Martin KelloDepartment of Pharmacology, Faculty of Medicine, Pavol Jozef Šafárik University, 040 11 Košice, Slovakia.ORCID 0000-0002-2454-5799
Radka MichalkováDepartment of Pharmacology, Faculty of Medicine, Pavol Jozef Šafárik University, 040 11 Košice, Slovakia.ORCID 0000-0002-9987-1556
Olga WesołowskaDepartment of Biophysics and Neurobiology, Wroclaw Medical University, 50-369 Wrocław, Poland.ORCID 0000-0003-1659-3288
Kamila Środa-PomianekDepartment of Biophysics and Neurobiology, Wroclaw Medical University, 50-369 Wrocław, Poland.ORCID 0000-0003-3454-5044
Sérgio M MarquesLoschmidt Laboratories, Department of Experimental Biology and RECETOX, Faculty of Science, Masaryk University, 625 00 Brno, Czech Republic.ORCID 0000-0002-6281-7505
David BednářLoschmidt Laboratories, Department of Experimental Biology and RECETOX, Faculty of Science, Masaryk University, 625 00 Brno, Czech Republic.
Viktória HázikováDepartment of Pharmacology, Faculty of Medicine, Pavol Jozef Šafárik University, 040 11 Košice, Slovakia.
Tomáš Ján LiškaInstitute of Chemistry, Faculty of Science, Pavol Jozef Šafárik University, 040 11 Košice, Slovakia.ORCID 0009-0007-8179-1316
Viera HabalováDepartment of Medical Biology, Faculty of Medicine, Pavol Jozef Šafárik University, 040 11 Košice, Slovakia.

Funding

European Union's Horizon 2020 Research and Innovation Programme 101136607European Union's Horizon 2020 Research and Innovation Programme 857560Grant Agency of the Ministry of the Education, Science, Research and Sport of the Slovak Republic VEGA 1/0446/22Ministry of Education, Youth and Sports of the Czech Republic LM2018140Ministry of Education, Youth and Sports of the Czech Republic LM2023055National Institute for Cancer Research (Programme EXCELES) LX22NPO5102VVGS UPJŠ 2024-2025 Interdisciplinary Research Projects for University Teachers, Researchers Under 35, and PhD Students VVGS-2023-2754
6 · The paper itself

Abstract

Chalcones, potential anticancer agents, have shown promise in the suppression of multidrug resistance due to the inhibition of drug efflux driven by certain adenosine triphosphate (ATP)-binding cassette (ABC) transporters. The gene and protein expression of chosen ABC transporters (multidrug resistance protein 1, ABCB1; multidrug resistance-associated protein 1, ABCC1; and breast cancer resistance protein, ABCG2) in human colorectal cancer cells (COLO 205 and COLO 320, which overexpress active ABCB1) was mainly studied in this work under the influence of a novel synthetic acridine-based chalcone, 1C. While gene expression dropped just at 24 h, compound 1C selectively suppressed colorectal cancer cell growth and greatly lowered ABCB1 protein levels in COLO 320 cells at 24, 48, and 72 h. It also reduced ABCC1 protein levels after 48 h. Molecular docking and ATPase tests show that 1C probably acts as an allosteric modulator of ABCB1. It also lowered galectin-1 (GAL1) expression in COLO 205 cells at 24 h. Functional tests on COLO cells revealed ABCB1 and ABCC1/2 to be major contributors to multidrug resistance in both. Overall, 1C transiently lowered GAL1 in COLO 205 while affecting important functional ABC transporters, mostly ABCB1 and to a lesser extent ABCC1 in COLO 320 cells. COLO 320's absence of GAL1 expression points to a possible yet unknown interaction between GAL1 and ABCB1.

Indexed as

AcridinesAntineoplastic AgentsATP-Binding Cassette TransportersChalconeChalconesATP-Binding Cassette, Sub-Family C ProteinsATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily G, Member 2Cell Line, TumorCell ProliferationColorectal NeoplasmsDrug Resistance, NeoplasmGene Expression Regulation, NeoplasticHumansMolecular Docking SimulationMultidrug Resistance-Associated Protein 2ABCB1 protein, humanABCC2 protein, humanAcridinesAntineoplastic AgentsATP-Binding Cassette, Sub-Family C ProteinsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily G, Member 2ChalconeChalconesmultidrug resistance-associated protein 1Multidrug Resistance-Associated Protein 2ABCB1ABCC1ABCG2chalconecolorectal carcinomadrug effluxexpressiongalectin-1multidrug resistancetransporter

Identifiers

PMID40362377
PMCPMC12071533

What Socratic holds

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.